Biliatresone, as well as preparation method, medicinal composition and application thereof

A composition and compound technology, applied in the field of medicine, can solve the problems of limiting the in-depth study of animal models of biliary atresia, the single origin of raw materials of Biliatresone, and the slow progress in the exploration of the pathogenesis and prevention methods of biliary atresia

Inactive Publication Date: 2019-04-09
CHILDRENS HOSPITAL OF FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, at present, due to many factors such as single origin of raw materials for extraction of natural biliatresone, complex purification technology, and low yield, the in-depth research on animal models of biliary atresone induced by biliatresone is greatly limited, resulting in slow progress in the industry's exploration of the pathogenesis and prevention methods of biliary atresia

Method used

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  • Biliatresone, as well as preparation method, medicinal composition and application thereof
  • Biliatresone, as well as preparation method, medicinal composition and application thereof
  • Biliatresone, as well as preparation method, medicinal composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Synthesis of Biliatresone Compounds

[0026] According to the following synthetic route:

[0027]

[0028] The first step: TBSCl (4.3g, 28.5mmol) dissolved in 10 milliliters of DCM was added dropwise to compound 1 (synthetic references Clarke, Aimee K.; James, Michael J.; etal.Angewandte Chemie- International Edition, 2016, vol.55, #44p.13798-13802) (3.7g, 18.9mmol) and 70ml of DCM solution of imidazole (2.59g, 38mmol), the addition was completed in about 30 minutes, and it rose naturally to Reacted at room temperature overnight, TLC raw materials reacted completely, filtered, the filtrate was washed with water, separated, the organic phase was dried and passed through the column to obtain the product compound 2, 5 g, the yield was 85%, and the appearance was a colorless oil;

[0029] The second step: compound 3 (540mg, 2.06mmol) (synthetic references Shuji Jinno, TakaakiOkit, and Kuniyo Inouye, Bioorganic & Medicinal Chemistry Letters 9 (1999) 1029-1032) ...

Embodiment 2

[0032] Embodiment 2 animal experiments

[0033] The compound Biliatresone, as a biliary epithelial drug, was used to induce biliary atresia in animal models.

[0034] Set up a concentration gradient of Biliatresone, respectively 0.1μg / ml, 0.15μg / ml, 0.2μg / ml, and the control group to treat the zebrafish larvae 5 days after fertilization for 24h and 48h, and feed the long-chain fatty acid Bodipy- C16 (0.2μg / ml), using a fluorescent microscope to photograph the development of the gallbladder and intestinal tract;

[0035]The results showed that as the concentration of Biliatresone increased and the treatment time increased, gallbladder development disorders appeared in zebrafish larvae, and the gallbladder of zebrafish larvae disappeared after 0.2 μg / ml Biliatresone treatment for 24 hours and 0.15 μg / ml Biliatresone treatment for 48 hours. The results confirmed that the prepared The compound Biliatresone is biologically active.

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Abstract

The invention belongs to the technical field of medicines, and relates to Biliatresone separated and purified from plants, as well as a preparation method, medicinal composition and application thereof. The Biliatresone further comprises cis-trans-isomer, enantiomer, diastereoisomer, raceme, solvate, hydrate or pharmaceutically acceptable salt and ester. Bioactivity experimental tests indicate that the compound can be used for remarkably inhibiting zebrafish larvae from gallbladder dysplasia, and prove that the compound Biliatresone has bioactivity, can be further used as biliary epithelia-philic medicines for studying biliary atresia inducing animal models.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to extrahepatic biliary tract toxin Biliatresone isolated and purified from plants, a preparation method, a pharmaceutical composition and application thereof. The biological activity test shows that this kind of compound can significantly inhibit the gallbladder development disorder in zebrafish larvae, and it is confirmed that the prepared compound Biliatresone has biological activity, and can be further used as a drug for biliary epithelial cells, and can be used to induce biliary atresia in animal models. Background technique: [0002] The prior art discloses that biliary atresia (BA) is the most common cholestatic disease in children. The disease is characterized by progressive inflammation and fibrous obstruction of extrahepatic and extrahepatic bile ducts. Clinical practice shows that without surgical treatment, Affected children usually die before the age of 2. Some studies...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D317/64A61K31/36A61P1/16
CPCC07D317/64
Inventor 郑珊董瑞杨一凡
Owner CHILDRENS HOSPITAL OF FUDAN UNIV
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